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| 5mg |
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| 25mg |
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| 100mg |
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Purity: ≥98%
Chidamide (CS-055, Tucidinostat, HBI-8000; trade name: Epidaza), is a potent and orally bioavailable benzamide-type histone deacetylase (HDAC) inhibitor with IC50s of 95, 160, 67 and 78 nM for HDAC1, HDAC2, HDAC3 and HDAC10, respectively. Chidamide is classified as an orphan drug in Japan and is approved by the Chinese FDA for the treatment of relapsed or refractory peripheral T-cell lymphoma (PTCL). It's only legal in China as of April 2015. The selective binding and inhibition of HDAC by chindamide causes the histone protein H3 to become more acetylated. Additionally, it suppresses the expression of signaling kinases in the MAPK/Ras and PI3K/Akt signaling pathways. In addition, it may cause cell cycle arrest and induce tumor cell apoptosis, which may stop the growth of tumor cells in tumor cells that are vulnerable to it. Research is being done on chidamide as a potential pancreatic cancer treatment. It is not, however, approved by the US FDA for the treatment of pancreatic cancer.
| Targets |
HDAC3 (IC50 = 67 nM); HDAC10 (IC50 = 78 nM); HDAC1 (IC50 = 95 nM); HDAC2 (IC50 = 160 nM); HDAC11 (IC50 = 432 nM); HDAC8 (IC50 = 733 nM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The Colorimetric HDAC Activity Assay kit's instructions are followed to detect HDAC activity. HDAC substrate and nuclear protein (50 μg) extract from leukemia cells are added to each reaction (100 μL). Chidamide (CS055) and MS-275 are added to the mixtures and incubated at 37°C for one hour in order to test the impact of HDACis. A microplate reader is used to measure the HDAC activities at 405 nm. The double-distilled water containing 10 μM Trichostatin A, a known strong HDACi, is used as a negative control and set to 0%, while the positive control (only nuclear extract and vehicle) is set to 100%.
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| Cell Assay |
Chidamide is added to isolated PBMC effector cells in 6-well plates (6 x 106 cells/well) for varying durations of time (24-72 hours) at varying concentrations (0-400 nM).
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| Animal Protocol |
Athymic nude mice (BALB/c-nu)
12.5-50 mg/kg oral |
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| References | ||
| Additional Infomation |
Chidamide is a member of benzamides.
Tucidinostat is an investigational drug that is being studied as part of a strategy to cure HIV infection. Tucidinostat belongs to a group of HIV drugs called latency-reversing agents. Tucidinostat is an orally bioavailable benzamide-type inhibitor of histone deacetylase (HDAC) isoenzymes 1, 2, 3 and 10, with potential antineoplastic activity. Upon administration, tucidinostat binds to and inhibits HDACs, leading to an increase of acetylation levels of histone proteins. This agent also inhibits the expression of kinases in the PI3K/Akt and MAPK/Ras signaling pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis. This may inhibit tumor cell proliferation in susceptible tumor cells. HDACs, a class of enzymes that deacetylate chromatin histone proteins, are upregulated in many tumor types and play key roles in gene expression. Compared to some other benzamide-type HDAC inhibitors, chidamide is more stable, more resistant to degradation and has a longer half-life. Drug Indication Investigated for use/treatment in cancer/tumors (unspecified). Mechanism of Action Chidamide is an orally bioavailable histone deacetylase (HDAC) inhibitor derived from the benzamide class. Histone deacetylase inhibitors are a class of cancer drugs that induce selective regulation of gene expression in cancer cells. [HUYA Biosciences Press Release] |
| Molecular Formula |
C22H19FN4O2
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| Molecular Weight |
390.41
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| Exact Mass |
390.149
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| CAS # |
1616493-44-7
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| Related CAS # |
Tucidinostat-d4
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| PubChem CID |
12136798
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| Appearance |
White to off-white solid
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
602.1±55.0 °C at 760 mmHg
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| Flash Point |
317.9±31.5 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.691
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
577
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC(=C(C=1)N)NC(C1C=CC(=CC=1)CNC(/C=C/C1C=NC=CC=1)=O)=O
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| InChi Key |
SZMJVTADHFNAIS-BJMVGYQFSA-N
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| InChi Code |
InChI=1S/C22H19FN4O2/c23-18-8-9-20(19(24)12-18)27-22(29)17-6-3-16(4-7-17)14-26-21(28)10-5-15-2-1-11-25-13-15/h1-13H,14,24H2,(H,26,28)(H,27,29)/b10-5+
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| Chemical Name |
N-(2-amino-4-fluorophenyl)-4-[[[(E)-3-pyridin-3-ylprop-2-enoyl]amino]methyl]benzamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% CMC Na: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5614 mL | 12.8070 mL | 25.6141 mL | |
| 5 mM | 0.5123 mL | 2.5614 mL | 5.1228 mL | |
| 10 mM | 0.2561 mL | 1.2807 mL | 2.5614 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05140616 | Recruiting | Drug: Chidamide | Safety and Efficacy | The First Affiliated Hospital of Soochow University |
May 31, 2021 | Phase 1 Phase 2 |
| NCT05951855 | Recruiting | Drug: Selinexor Drug: Chidamide |
Acute Myeloid Leukemia (Relapsed/Refractory) |
The First Affiliated Hospital of Soochow University |
October 19, 2022 | Phase 2 |
| NCT05330364 | Recruiting | Drug: Chidamide Drug: Cladribine |
Acute Myeloid Leukemia | Ge Zheng | June 1, 2021 | Phase 2 |
| NCT05270200 | Recruiting | Drug: Azacitidine Drug: Chidamide |
Leukemia, Myeloid, Acute | Zhujiang Hospital | February 1, 2022 | Phase 1 Phase 2 |
| NCT04994210 | Recruiting | Drug: Sintilimab Drug: Chidamide |
Safety and Efficacy | Sun Yat-sen University | October 4, 2021 | Phase 2 |
 Expression levels of MEG3 and methylation related genes in different stages of CML and in healthy donors and the methylation status of MEG3 in different stages of CML and in healthy donors.EBioMedicine.2018 Aug;34:61-75. |
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 Changes in mRNA and protein levels in CML blast cells after chidamide treatment.EBioMedicine.2018 Aug;34:61-75. |
 Changes in mRNA and protein levels in CML blast cells after chidamide treatment.EBioMedicine.2018 Aug;34:61-75. |
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